Bioactivation mechanisms of N‐hydroxyaristolactams: Nitroreduction metabolites of aristolochic acids
Sign Up to like & getrecommendations! Published in 2019 at "Environmental and Molecular Mutagenesis"
DOI: 10.1002/em.22321
Abstract: Aristolochic acids (AAs) are human nephrotoxins and carcinogens found in concoctions of Aristolochia plants used in traditional medicinal practices worldwide. Genotoxicity of AAs is associated with the formation of active species catalyzed by metabolic enzymes,… read more here.
Keywords: strains expressing; aristolochic acids; expressing human; mechanisms hydroxyaristolactams ... See more keywords
Detoxification of benzo[a]pyrene primarily depends on cytochrome P450, while bioactivation involves additional oxidoreductases including 5‐lipoxygenase, cyclooxygenase, and aldo‐keto reductase in the liver
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Biochemical and Molecular Toxicology"
DOI: 10.1002/jbt.21902
Abstract: Cytochrome P450s are involved in detoxification and activation of benzo[a]pyrene (BaP) with unclear balance and unknown contribution of other oxidoreductases. Here, we investigated the BaP and BaP‐induced mutagenicity in hepatic and extra‐hepatic tissues using hepatic… read more here.
Keywords: reductase; gpt mice; detoxification; benzo pyrene ... See more keywords
Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.09.038
Abstract: Ethionamide is a key antibiotic prodrug of the second-line chemotherapy regimen to treat tuberculosis. It targets the biosynthesis of mycolic acids thanks to a mycobacterial bioactivation carried out by the Baeyer-Villiger monooxygenase EthA, under the… read more here.
Keywords: efficient analoging; around ethionamide; bioactivation; ethionamide explore ... See more keywords
Meloxicam methyl group determines enzyme specificity for thiazole bioactivation compared to sudoxicam.
Sign Up to like & getrecommendations! Published in 2020 at "Toxicology letters"
DOI: 10.1016/j.toxlet.2020.11.015
Abstract: Meloxicam is a thiazole-containing NSAID that was approved for marketing with favorable clinical outcomes despite being structurally similar to the hepatotoxic sudoxicam. Introduction of a single methyl group on the thiazole results in an overall… read more here.
Keywords: sudoxicam; methyl group; group; bioactivation ... See more keywords
Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical research in toxicology"
DOI: 10.1021/acs.chemrestox.1c00426
Abstract: Sunitinib is an orally administered tyrosine kinase inhibitor associated with idiosyncratic hepatotoxicity; however, the mechanisms of this toxicity remain unclear. We have previously shown that cytochromes P450 1A2 and 3A4 catalyze sunitinib metabolic activation via… read more here.
Keywords: sunitinib; bioactivation; p450 activity; p450 ... See more keywords
Modulation of Cytotoxicity by Transcription-Coupled Nucleotide Excision Repair Is Independent of the Requirement for Bioactivation of Acylfulvene.
Sign Up to like & getrecommendations! Published in 2017 at "Chemical research in toxicology"
DOI: 10.1021/acs.chemrestox.6b00240
Abstract: Bioactivation as well as DNA repair affects the susceptibility of cancer cells to the action of DNA-alkylating chemotherapeutic drugs. However, information is limited with regard to the relative contributions of these processes to the biological… read more here.
Keywords: dna; bioactivation; transcription coupled; cytotoxicity ... See more keywords
Metabolite Profiling and Reaction Phenotyping for the in vitro Assessment of the Bioactivation of Bromfenac.
Sign Up to like & getrecommendations! Published in 2019 at "Chemical research in toxicology"
DOI: 10.1021/acs.chemrestox.9b00268
Abstract: Bromfenac is a non-steroidal anti-inflammatory drug that was approved and subsequently withdrawn from the market due to reported cases of acute hepatotoxicity. Recently, in vitro studies have revealed that bromfenac requires UDPGA and alamethicin supplemented… read more here.
Keywords: profiling reaction; bioactivation; metabolite profiling; bromfenac ... See more keywords
Characterization of reactive intermediates formation in dacomitinib metabolism and bioactivation pathways elucidation by LC-MS/MS: in vitro phase I metabolic investigation
Sign Up to like & getrecommendations! Published in 2018 at "RSC Advances"
DOI: 10.1039/c8ra06709k
Abstract: Dacomitinib (DCB) is a second generation irreversible tyrosine kinase inhibitor (TKI) that is claimed to overcome the disadvantages of the resistance developed by the first line epidermal growth factor receptor (EGFR) TKIs. In the current… read more here.
Keywords: vitro phase; characterization reactive; bioactivation; reactive intermediates ... See more keywords
Novel advances in biotransformation and bioactivation research—2019 year in review*
Sign Up to like & getrecommendations! Published in 2020 at "Drug Metabolism Reviews"
DOI: 10.1080/03602532.2020.1772281
Abstract: Abstract Biotransformation is one of the main mechanisms used by the body to eliminate drugs. As drug molecules become more complicated, the involvement of drug metabolizing enzymes increases beyond those that are typically studied, such… read more here.
Keywords: year; novel advances; drug; biotransformation ... See more keywords
Bioactivation and reactivity research advances – 2021 year in review
Sign Up to like & getrecommendations! Published in 2022 at "Drug Metabolism Reviews"
DOI: 10.1080/03602532.2022.2097254
Abstract: Abstract This year’s review on bioactivation and reactivity began as a part of the annual review on biotransformation and bioactivation led by Cyrus Khojasteh (see references). Increased contributions from experts in the field led to… read more here.
Keywords: year; bioactivation; review; bioactivation reactivity ... See more keywords
Identification of reactive intermediate formation and bioactivation pathways in Abemaciclib metabolism by LC–MS/MS: in vitro metabolic investigation
Sign Up to like & getrecommendations! Published in 2019 at "Royal Society Open Science"
DOI: 10.1098/rsos.181714
Abstract: Abemaciclib (Verzenio®) is approved as a tyrosine kinase inhibitor (TKI) for breast cancer treatment. In this study, in vitro phase I metabolic profiling of Abemaciclib (ABC) was done using rat liver microsomes (RLMs). We checked… read more here.
Keywords: vitro metabolic; metabolism; identification reactive; formation ... See more keywords